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Eur J Med Chem. 2016 Jul 19;117:33-46. doi: 10.1016/j.ejmech.2016.03.089. Epub 2016 Apr 2.

5-Ene-4-thiazolidinones induce apoptosis in mammalian leukemia cells.

Author information

1
Institute of Cell Biology of National Academy of Sciences of Ukraine, 14/16 Drahomanov Str., Lviv 79005, Ukraine.
2
Danylo Halytsky Lviv National Medical University, 69 Pekarska Str., Lviv 79010, Ukraine.
3
Poznan University of Medical Sciences, 6 Grunwaldzka Str., Poznan 60780, Poland.
4
Danylo Halytsky Lviv National Medical University, 69 Pekarska Str., Lviv 79010, Ukraine. Electronic address: dr_r_lesyk@org.lviv.net.

Abstract

The article presents the synthesis of 5-ene-4-thiazolidinone derivatives with pyrazole core linked by enamine group. The structure and purity of compounds were confirmed by analytical and spectral data including X-ray analysis. Target compounds were screened for their anticancer activity and selective antileukemic action was confirmed. 5-[5-(2-Hydroxyphenyl)-3-phenyl-4,5-dihydropyrazol-1-ylmethylene]-3-(3-acetoxyphenyl)-2-thioxothiazolidin-4-one (compound 1) was selected as most active agent against HL-60 and HL-60/ADR cell lines; IC50 = 118 nM/HL-60 with low toxicity towards pseudonormal cells. The mitochondria-depended apoptosis was identified as the main mode of 1 action. Moreover compound's effect induces G0/G1 arrest of the treated cells and causes inhibition of cell division and is related with activation of ROS production.

KEYWORDS:

5-Ene-4-thiazolidinones; Anticancer activity; Apoptosis; Leukemia; ROS

PMID:
27089210
DOI:
10.1016/j.ejmech.2016.03.089
[Indexed for MEDLINE]

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